Expiration date: 03/2025

Release form and composition:

The tablets covered with a cover white or nearly white, kapsulovidnoy form, biconcave, with dividing line on one side on a break - white or nearly white.

1 tablet contains sertraline (hydrochloride) 50 or 100 mg

Excipients: microcrystalline cellulose, sodium carboxymethyl starch, calcium phosphate dihydrate, hydroxypropyl cellulose, polysorbate, magnesium stearate.

Pharmachologic effect:

Antidepressant. Selective serotonin reuptake inhibitor (5-HT). It has little effect on the reuptake of noradrenaline and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin human platelets. Sertraline has no affinity for muscarinic, serotonin, dopamine, adrenergic, histamine, GABA- or benzodiazepine receptors. It has no stimulating, sedative or anticholinergic action.

Antidepressant effect was seen at the end of the second week of the regular intake of sertraline, while the maximum effect is achieved only after 6 weeks.

Unlike tricyclic antidepressants, sertraline when assigning no increase in body weight. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics:

Suction

After oral administration of sertraline absorption from the gastrointestinal tract is large, but is slow. Cmax achieved through 4.5-8.4 h in plasma. The bioavailability during a meal increased by 25%, while the time to reach Cmax is shortened.

Distribution

With a single daily reception Css plasma levels achieved within a week. sertraline Plasma protein binding is 98%. Vd gt20 l / kg.

Sertraline is excreted in breast milk. Data on its permeability through the placental barrier there.

Metabolism and excretion

Sertraline is extensively metabolized during the first passage through the liver, subjected to N-demethylation. Its main metabolite - N-desmetilsertralin less active as compared to the parent compound. The metabolites are excreted with urine and faeces in equal amounts. About 0.2% of sertraline excreted by the kidneys unchanged. T1 / 2 of 22-36 hours, and is not dependent on age or gender. For N-desmetilsertralina this figure is 62-104 hours.

Pharmacokinetics in special clinical situations

If you violate the T1 / 2 and AUC increased liver function.

Regardless of the degree of severity of renal insufficiency pharmacokinetics of sertraline when applied constant does not change.

Sertraline not dialysed.

Testimony:

• Depression different etiology (treatment and prevention)
  
• Obsessive-Compulsive Disorder (OCD)
  
• Panic disorder (with or without agoraphobia)
  
• Post-traumatic stress disorder (PTSD).
  

Dosage and administration:

Adults with depression and OCD drug is administered in an initial dose of 50 mg 1 time / day in the morning or in the evening. The daily dose can be gradually, not earlier than one week increased to a maximum of 50 mg daily dose of 200 mg.

When panic disorder and PTSD starting dose is 25 mg 1 time / day in the morning or in the evening. After one week the dose can be increased to 50 mg 1 time / day, and then gradually, not earlier than one week, the daily dose can be increased to a maximum of 50 mg daily dose of 200 mg.

Satisfactory therapeutic results achieved typically after 7 days of starting treatment. However, to achieve full therapeutic effect requires the regular intake of the drug for 2-4 weeks. In the treatment of OCD in order to achieve a good result may require 8-12 weeks. The minimum dose providing therapeutic effect is retained as a supporting hereinafter.

Children with OCD drug is prescribed depending on the age. For children aged 6 to 12 years of the initial dose is 25 mg 1 time / day in the morning or in the evening. After one week the dose can be increased to 50 mg 1 time / day. For children and adolescents aged 12 to 17 years starting dose is 50 mg 1 time / day, morning or evening. The daily dose can be gradually, not earlier than one week, increasing to 50 mg up to a maximum daily dose of 200 mg. To avoid overdose, should be considered a lower body weight in children compared with adults and with increasing doses of over 50 mg / day should be carefully monitored for this category of patients, and the first signs of an overdose of the drug to cancel.

In elderly patients a special dose adjustment is required.

In severe hepatic dysfunction dose should be reduced or increased intervals between doses.

Patients with impaired renal function, a special dose adjustment is required.

Side effects:

From the digestive system: dry mouth, decreased appetite (rarely - increased) up to anorexia, diarrhea disorders (flatulence, nausea, vomiting, diarrhea), abdominal pain, long-term use in 0.8% of cases - asymptomatic increase of transaminase activity in serum blood (to remove the drug there is a normalization of enzyme activity).

From the central and peripheral nervous system: drowsiness, headache, dizziness, tremors, insomnia, anxiety, agitation, hypomania, mania, abnormal gait, weakness during treatment with sertraline were marked extrapyramidal disorder, dyskinesia, tremor, seizures, visual disturbances. Movement disorders were more common in patients with indications of their presence in the history or concomitant use of antipsychotics.

From endocrine system: ejaculation disorder, decreased libido, menstrual disorders, hyperprolactinemia, galactorrhea.

On the part of metabolism: increased sweating, weight loss of 0.8% (mostly in elderly patients, as well as when taking diuretics or some other drugs) - transient hyponatremia (this side effect associated with the syndrome of inappropriate secretion of ADH).

Dermatological reactions: redness, skin rash, rarely - erythema multiforme.

Upon termination of treatment: rarely - withdrawal syndrome: possible paresthesia, gipostezii, depressive symptoms, hallucinations, aggressive reaction, agitation, anxiety or psychotic symptoms that are indistinguishable from symptoms of the underlying disease.

Contraindications:

• Unstable epilepsy
  
• Children up to age 6 years
  
• pregnancy
  
• Lactation
  
• Concomitant use of sertraline and MAO inhibitors (for the replacement of one drug to another should avoid antidepressants within 14 days)
  
• Concomitant use of sertraline with tryptophan or fenfluramine
  
• Hypersensitivity to the drug.
  

With care use in patients with organic brain disorders (including with mental retardation), manic states, epilepsy, liver and / or kidney failure, reduction of body weight.

Pregnancy and lactation:

Adequate and well-controlled clinical studies safety Serenata drug during pregnancy has not been. Appointment of the drug is contraindicated for pregnant women.

Women of reproductive age, who is supposed to conduct treatment with Serenata, must use effective contraceptive methods.

Sertraline is excreted in breast milk. Reliable data on the safety of sertraline during lactation are not available. Therefore, breastfeeding should be discontinued, if necessary, the appointment of the drug.

Special instructions:

Sertraline should not be administered within 14 days after discontinuation of treatment MAO inhibitors. MAO inhibitors are not appointed within 14 days after discontinuation of sertraline.

In patients receiving electroconvulsive therapy is not enough experience with the drug Serenata. The possible success or the risk of such combined treatment has not been studied.

Patients with depression are at risk for suicide attempts. This risk persists until the development of remission. Therefore, from the beginning of the treatment and to achieve optimal clinical response for patients should establish a permanent medical supervision.

With the simultaneous use of the drug Serenata and drugs that have a depressant effect on the central nervous system, require special care and careful monitoring of the patient's condition.

Use in Pediatrics

Precautions should use the drug in children under the age of 6 years.

During treatment, the use of alcohol is forbidden.

Effects on ability to drive vehicles and management mechanisms

Appointment of sertraline is usually not accompanied by violation of psychomotor functions. However, its use in conjunction with other drugs may impair attention and motor coordination. Therefore, during treatment with sertraline drive vehicles, special equipment or practice associated with an increased risk of the activity is not recommended.

Overdose:

Symptoms: not revealed severe symptoms of sertraline overdose, even in the appointment of the drug in high doses. However, severe poisoning can occur when taken with other drugs or ethanol. Overdose can cause serotonin syndrome with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, agitation, diarrhea, sweating, myoclonus and hyperreflexia.

Treatment: No specific antidote. It requires intensive supportive care and constant monitoring of vital body functions. Induce vomiting is not recommended. Introduction of the activated carbon can be more effective than gastric lavage. It is necessary to maintain airway patency. In sertraline large Vd, thus increasing diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective.

Drug Interactions:

With simultaneous use of the drug Serenata and MAO inhibitors as selectively acting (selegiline) and a reversible type of action (moclobemide) may develop severe complications, including serotonin syndrome. Similar complications, sometimes fatal, occur in the appointment of MAO inhibitors during treatment with antidepressants, depressing neuronal uptake of monoamines or immediately after their withdrawal. With simultaneous use of selective inhibitors of reverse neuronal uptake of serotonin and MAO inhibitors arise: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), mental status changes, including increased irritability, marked agitation, confusion, which in some cases may go into state delirious or coma.

The joint appointment of coumarin derivatives and sertraline showed a significant increase in prothrombin time (it is recommended to monitor the prothrombin time at the beginning of treatment with Serenata and after its cancellation).

Pharmacokinetic interactions

Sertraline is bound to plasma proteins. Therefore, it must consider the possibility of interaction with other drugs that bind to proteins (for example, diazepam, warfarin and tolbutamide) is needed.

In an application with cimetidine observed a significant decrease in sertraline clearance. Long-term treatment with sertraline 50 mg / day in the case of simultaneous application there is an increase in plasma concentrations of desipramine, which is metabolized with the participation of isoenzyme CYP2D6.

In experimental studies on drug interactions in vitr shown that the metabolic processes that take place with the participation isozymes CYP3A3 / 4 - beta-hydroxylation of endogenous cortisol and metabolism of carbamazepine and terfenadine - do not change during long-term administration of sertraline at a dose of 200 mg / day. The concentration in the blood plasma tolbutamide, warfarin and phenytoin prolonged assignment of sertraline in the same dose also varies. Thus, we can conclude that sertraline does not inhibit the activity of CYP2C9 isoenzymes.

Sertraline not affect the diazepam concentration in the serum, indicating no inhibition of CYP2C19 isozyme.

According to studies in vitr sertraline has virtually no effect or minimally inhibits isoenzyme CYP1A2.

The pharmacokinetics of lithium does not change, while the use of sertraline, but in such cases there is often a tremor. As well as the appointment of other selective inhibitors of reverse neuronal serotonin reuptake, sertraline joint application with drugs that affect the serotonergic transmission (eg, lithium), requires increased caution. When replacing one inhibitor of neuronal uptake of serotonin on the other in a period of no need of laundering. However, you want to be careful with changes in the course of treatment.

Avoid concomitant administration of tryptophan or fenfluramine with sertraline.

Sertraline causes minimal induction of microsomal liver enzymes. Co-administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T1 / 2 antipyrine, although there is only 5% of cases.

With simultaneous use of sertraline does not alter the beta-adrenoceptor blocking action of atenolol.

With simultaneous use of sertraline at a dose of 200 mg / day with glibenclamide or digoxin drug interactions have been identified.

Conditions and terms:

The drug should be stored out of reach of children, at a temperature below 25 ° C. Shelf life - 2 years.